C07D215/233

Salt Forms of a Kinase Inhibitor

The present invention relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid crystalline salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.

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Compounds for the Treatment of Kinase-Dependent Disorders
20230043835 · 2023-02-09 ·

Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Ax1 and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.

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Compounds for the Treatment of Kinase-Dependent Disorders
20230043835 · 2023-02-09 ·

Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Ax1 and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.

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Pleuromulin 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid ester with antibacterial activity and a method of preparing the same

A compound with anti-drug resistant bacteria activity having the following formula (I): ##STR00001##
is disclosed. The methods of preparing the compound of formula (I) are also disclosed.

Pleuromulin 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid ester with antibacterial activity and a method of preparing the same

A compound with anti-drug resistant bacteria activity having the following formula (I): ##STR00001##
is disclosed. The methods of preparing the compound of formula (I) are also disclosed.

ENZYME AND RECEPTOR MODULATION

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

ENZYME AND RECEPTOR MODULATION

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer
20180002289 · 2018-01-04 ·

Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide.

Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer
20180002289 · 2018-01-04 ·

Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide.

QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF

This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R.sup.4, R.sup.q, o, R.sup.A, W and R.sup.B and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.

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